Department of Biomedical and Molecular Sciences, Queen's University, Kingston, Ontario K7L 3N6, Canada.
Department of Chemistry, Queen's University, Kingston, Ontario K7L 3N6, Canada.
Bioorg Med Chem. 2020 Jun 1;28(11):115494. doi: 10.1016/j.bmc.2020.115494. Epub 2020 Apr 10.
A series of compounds was designed and synthesized having two imidazolium rings separated by a polymethylene spacer and having alkyl substituents on each of the imidazolium rings. The compounds were assayed for their effects on the activity of galactosyltransferase WbwC, and also on the growth of Gram-negative and Gram-positive bacteria, as well as human cells. The inhibition observed on enzyme activities and cell growth was dependent on the total number of carbons in the spacer and the alkyl substituents on the imidazolium rings. These readily synthesized, achiral compounds have potential as antimicrobial and antiseptic agents.
设计并合成了一系列化合物,这些化合物具有两个由聚亚甲基间隔基隔开的咪唑鎓环,并且每个咪唑鎓环上都有烷基取代基。测试了这些化合物对半乳糖基转移酶 WbwC 的活性以及对革兰氏阴性和革兰氏阳性细菌以及人细胞生长的影响。观察到的对酶活性和细胞生长的抑制作用取决于间隔基中的碳原子总数和咪唑鎓环上的烷基取代基。这些易于合成的非手性化合物具有作为抗菌和防腐剂的潜力。